| Literature DB >> 9871716 |
A E Weber1, R J Mathvink, L Perkins, J E Hutchins, M R Candelore, L Tota, C D Strader, M J Wyvratt, M H Fisher.
Abstract
A cloned human beta 3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM beta 3 agonist which shows 30-fold selectivity for beta 3 agonist activity over beta 1 and beta 2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over beta 1 and beta 2, respectively.Entities:
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Year: 1998 PMID： 9871716 DOI： 10.1016/s0960-894x(98)00169-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823